Global Patent Index - EP 0331080 A2

EP 0331080 A2 19890906 - Imidazole derivatives, process for production thereof, and use thereof.

Title (en)

Imidazole derivatives, process for production thereof, and use thereof.

Title (de)

Imidazol-Derivate, Verfahren zu deren Herstellung und ihre Verwendung.

Title (fr)

Dérivés d'imidazole, procédé pour leur préparation et leur utilisation.

Publication

EP 0331080 A2 19890906 (EN)

Application

EP 89103404 A 19890227

Priority

  • JP 4692188 A 19880229
  • JP 8208988 A 19880401
  • JP 8209088 A 19880401

Abstract (en)

Disclosed are imidazole derivatives represented by formula [I]: <CHEM> wherein R is a hydrogen atom or <CHEM> wherein R<2> is a hydrogen atom or a hydroxy protecting group, R<2> protecting either a single hydroxy or two hydroxies together when R<2> is a hydroxy protecting group, and R<3> is a hydrogen atom or OR<2>; A is CONH2 or CN; and R<1> is a hydrogen atom, lower alkyl, hydroxy lower alkyl, or phenyl. Also disclosed are six processes for producing these novel compounds among which a typical process comprises reacting a starting imidazole compound having a halogen at the 5-position thereof with an acetylene derivative to alkynylate the 5-position. Furthermore, the compounds have remarkable antitumor activities and therefore can provide novel antitumor agents.

IPC 1-7

A61K 31/415; A61K 31/70; C07D 233/90; C07H 19/052

IPC 8 full level

C07D 233/90 (2006.01); C07H 19/052 (2006.01)

CPC (source: EP KR US)

C07D 233/90 (2013.01 - EP US); C07H 17/02 (2013.01 - KR); C07H 19/052 (2013.01 - EP US); Y02P 20/55 (2015.11 - EP US)

Designated contracting state (EPC)

AT BE CH DE ES FR GB GR IT LI LU NL SE

DOCDB simple family (publication)

EP 0331080 A2 19890906; EP 0331080 A3 19901122; CA 1317588 C 19930511; KR 890013048 A 19890921; US 5059590 A 19911022; US 5126361 A 19920630

DOCDB simple family (application)

EP 89103404 A 19890227; CA 592209 A 19890227; KR 890002470 A 19890228; US 31696989 A 19890228; US 70221091 A 19910515